Design and synthesis of 4-acetoxypentanamide derivatives of spliceostatin A and their biological evaluation towards prostate cancer treatment
Bioorganic & Medicinal Chemistry Letters(2023)
Abstract
We designed and synthesized novel 4-acetoxypentanamide derivatives of spliceostatin A, whose 4-acetoxypente-namide moiety is reduced (7), isomerized (8), or substituted with methyl at the & alpha;-position (9). The results of biological evaluation against AR-V7 and the docking analysis of each derivative suggest that the geometry of the 4-acetoxypentenamide moiety of spliceostatin A is important for its biological activity.
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Key words
Prostate cancer,Splicing variant,Spliceostatin A,Michael acceptor
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